METHOD FOR IDENTIFYING AN ALLOSTERIC EFFECTOR OF A RECEPTOR

• Main Authors: HIBERT, MARCEL, GALZI, JEAN-LUC, BOURGUIGNON, JEAN-JACQUES, MAILLET, EMELINE
• Format: Patent
• Language: English; French; German
• Published: 16.03.2005
• Edition: 7
• Subjects: CHEMISTRY; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; TESTING

Method for detecting an allosteric effector (I) of a receptor (R). Method for detecting an allosteric effector (I) of a receptor (R) comprises determining the variation of: (1) the kinetics of dissociation and/or association of the complex formed between R and its ligand (L); and/or (2) the amplitude of the binding between R and L, in presence of (I), relative to that in absence of (I). If the variation in amplitude is negative, then the variation is kinetics must also be measured. R and L are implicated in at least one biological response, under appropriate physiological conditions, and (I) modulates at least one such response. R is labeled with a fluorescent protein (FP), derived from cnidarians, or its derivative, having molar extinction coefficient over 14000 M to the power of -1 cm to the power of -1 and quantum yield of fluorescence over 0.38. L is labeled with: (1) an agent (A) that absorbs light emitted from FP; or (2) a fluorescent substance (FS). The measurement of variation in kinetics/binding is based on fluorescent energy transfer (FET) between (a) FP and FS, which is either excited at the emission wavelength of FP or emits at the wavelength of excitation of FP, or (b) FP and (A). An Independent claim is also included for 23 new compounds (X) identified by the new method.